选择性5-羟色氨受体抑制剂——巴西苏木红素(英文)  

Brazilein,a Selective 5-HT Receptors Antagonist in Mouse Uterus

作　　者：王秀坤[1,2] 雷帆[1] 柴玉爽[1] 王玉刚[1] 詹宏磊[1] 邢东明[1] 游学甫[2] 李慧颖[1] 杜力军[1] 

机构地区：[1]清华大学生命科学学院医学院药物药理研究室,北京100084 [2]中国医学科学院北京协和医学院医药生物技术研究所药理室,北京100050

出　　处：《中国天然药物》2011年第5期338-344,共7页

基　　金：supported by the National S&T Major Special Project for New Drug R&D of China (Nos. 2009ZX09103-301, 2009ZX09502-021 and 2011ZX09101-002-11);the National Natural Science Foundation of China (Nos. 30973896,30801523 and 81073092);the Scientific Foundation for China Postdoctoral fellows (No. 20080440418);the Special Foundation for Laboratory of Tsinghua University (No. LF 20103579)~~

摘　　要：目的:子宫平滑肌内存在多种5-HT受体,5-HT通过作用于5-HT受体实现其对子宫收缩活性的影响。本研究探讨巴西苏木红素对5-HT受体的作用及其特点。方法:小鼠分离子宫平滑肌条,采用受体拮抗实验和real time PCR方法,对巴西苏木红素的5-HT受体的抑制作用进行研究。结果:巴西苏木红素虽然对正常子宫平滑肌的收缩幅度和频率无影响,但能明显抑制5-HT2受体激动剂马来酸麦角新碱的收缩活性,其pA2为5.71±0.21。而5-HT亚型的选择性激动剂舒马普坦(5-HT1D)、AL34662(5-HT2A)、MCPP(5-HT2C)的收缩子宫活性同样能够被巴西苏木红素抑制,pA2分别为4.58±0.06;4.91±0.15;5.38±0.15。巴西苏木红素明显抑制了5-HT受体1D和2C亚型mRNA的表达。结论:巴西苏木红素能够阻滞小鼠子宫5-HT受体,并通过可能影响5-HT受体所介导的子宫功能。AIM： To prove brazilein＇s effect on 5-HT receptor and to understand the characteristics of the action. METHODS： In this work, the blocking effect of brazilein on 5-HT receptor subtypes was investigated in isolated uterine strips using pharmacological （selective agonists） and molecular biological （real time PCR） approaches. RESULTS： brazilein does not affect the contractions of normal inice uterus, but inhibits uterine excitatory elicited by ergometrine maleate （pA2 = 5.71 ± 0.21）, a 5-HT2 receptor agonist. The excitatory effects of 5-HTID, 5-HT2A and 5-HT2c receptor agonists on uterus could be inhibited by brazilein （pA2 = 4.58 ± 0.06, 4.91 ± 0.15, 5.38± 0.15, respectively）. The mRNA expression of 5-HT1D and 5-HTzc receptors in mice uterus were decreased by brazilein. CONCLUSION： brazilein blocked 5-HT receptors in mice uterus and might affect the functions mediated by 5-HT receptors.

关 键 词：巴西苏木红素 5-HT受体 子宫 小鼠 

分 类 号：R965[医药卫生—药理学]